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Casein Kinase (CK) Inhibitors
 | | |  Casein kinases I and II (CKI and CKII) are highly conserved, ubiquitous serine/threonine protein kinases that play a significant role in neoplasma and cell survival. CKI can be found in the nucleus and the cytosol and is bound to the cytoskeleton and membranes. The CKI family consists of several isoforms (CKIa, b, g1, g2, g3, d and e) encoded by seven distinct genes. It plays a significant role in the regulation of circadian rhythm, intracellular trafficking and also acts as a regulator of Wnt & Hedgehog signalling, nuclear import, and the progression to Alzheimer's disease. CKII has traditionally been classified as a messenger-independent protein serine/threonine kinase that consists of two catalytic and two regulatory subunits. It plays an important role in the progression of the cell cycle and in maintenance of cell viability. It is highly conserved and is known to phosphorylate about 300 different proteins. CKII activity is required at transition points of the cell cycle. Excessive activity of CKII has been linked to oncogenic transformation and the development of primary and metastatic tumors. The development of CKII inhibitors may prove to be useful for an anti-cancer drug or to be used as a tool to dissect signalling pathways affected by CKII.
| | | | Product | Description | Casein Kinase I Inhibitor, D4476
Cat. No. 218696 | A cell-permeable triaryl substituted imidazolo compound that acts as a potent and relatively specific ATP-competitive inhibitor of CK1 (IC50 = 0.2 mM from S. pombe; 0.3 mM for CK1d) and ALK5 (IC50 = 0.5 mM). Purity: >95% by HPLC. | InSolution™ Casein Kinase I Inhibitor, D4476
Cat. No. 218705
| Supplied as a 10 mM (1 mg/251 ml) solution of Casein Kinase I Inhibitor, D4476 (Cat. No. 218696) in DMSO. Purity: >95% by HPLC. | Casein Kinase II Inhibitor I
Cat. No. 218697 | A cell-permeable, higly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2) (IC50 = 900 nM and 1.6 mM, using rat liver and human recombinant CK2, respectively) and DYRK (IC50 < 1 mM for DYRK1a). Purity: Single spot by TLC. CAS 17374-26-4. | InSolution™ Casein Kinase II Inhibitor I,
Cat. No. 218708
| Supplied as a 10 mM (5 mg/1.15 ml) solution of Casein Kinase II Inhibitor I (Cat. No 218697) in DMSO. Purity: Single spot by TLC. | Casein Kinase II Inhibitor II, DMAT
Cat. No. 218699 | A cell-permeable, potent, high affinity and ATP-competitive inhibitor of CK2 (IC50 = 140 nM for rat liver CK2; Ki = 40 nM). Displays ~1300 fold greater selectivity over CK1 (IC50 > 200 mM) and is superior to CK2 inhibitor, TBB (Cat. No 218697). Purity: >95% by HPLC. | InSolution™ Casein Kinase II Inhibitor II, DMAT
Cat. No. 218706
| Supplied as a 10 mM (5 mg/1.05 ml) solution of Casein Kinase II Inhibitor, DMAT (Cat. No. 218699) in DMSO. Purity: >95% by HPLC. | Casein Kinase II Inhibitor III, TBCA
Cat. No. 218710 | A cell-permeable, potent, selective and ATP-competitive inhibitor of Casein Kinase II (IC50 = 110 nM; IC50 for CKI > 40 mM). Purity: >95% by HPLC. | IC261
Cat. No. 400090 | A cell-permeable, potent and selective ATP-comptetitive inhibitor (IC50 = 0.7 - 1.3 mM and 0.6 - 1.4 mM for CKId and CKIe) |
| | | | | Related Resource  Inhibitor Resource | | | | | |
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